Fluorine-containing anthracycline derivatives having...

Details Fluorine-containing anthracycline derivatives having... Fluorine-containing anthracycline derivatives having...

C - Chemistry, Metallurgy

07

H

C07H 15/252 (2006.01) A61K 31/70 (2006.01)

Patent

CA 2184956

To provide novel fluorine-containing anthracycline derivatives having high antitumor activities and a solubility in water, there have now been synthesized a 7-0-(2,6-dideoxy- 2-fluoro-3-0- or -4-0- or -3,4-di-0-aminoalkanoyl-.alpha.-L- talopyranosyl)daunomycinone or -adriamycinone of general formula (I) shown below, as well as a 7-0-(3-0- or -4-0- or-3,4-di-0-aminoalkanoyl-2,6-dideoxy-2,6,6,6-tetraffluoro- .alpha.-L-talopyranosyl- or -2,6-dideoxy-6,6,6-trifluoro- lyxo-hexopyranosyl)adriamycinone of general formula (II) shown below:- General formula (I): (I) Image - 2 - General formula (II): Image (II) wherein either one or both of A1 and A is or are an .alpha.-amino acid residue or an .omega.-amino acid residue and T denotes a fluorine or hydrogen atom. The novel fluorine- containing anthracycline derivatives of general formulae (I) and (II) are highly active against tumors and soluble in water, and they are useful as antitumor agents administrable in the form of injectable solution.

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